Urokinase
From Proteopedia
(Difference between revisions)
(New page: {{STRUCTURE_3ig6| PDB=3ig6 | SIZE=400| SCENE= |right|CAPTION=Human urokinase A and B chains complex with inhibitor, 3ig6 }} '''Urokinase''' (UK) is a serine protease whose principa...) |
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| + | <StructureSection load='3ig6' size='350' side='right' caption='Human urokinase light chain fragment (pink) and catalytic domain (yellow) complex with inhibitor and phosphate, [[3ig6]]' scene='' > | ||
| + | == Function == | ||
| + | '''Urokinase''' (UK) or '''urokinase plasminogen activator''' or '''urokinase-type plasminogen activator''' is a serine protease whose principal substrate is plasminogen – the inactive zymogen of plasmin<ref>PMID:21711235</ref>. UK consists of 3 domains: ligand-binding domain and kringle and growth factor domains. Prourokinase (PUK) is the inactive zymogen of UK which becomes active by proteolytic cleavage into catalytic domain (residues 179-431) and short chain (residues 156-178). | ||
| - | + | == Relevance == | |
| - | + | Increased levels of UK are associated with poor prognosis in patients with breast cancer and thus is used as prognostic markers for the disease<ref>PMID:15944776</ref>. | |
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| + | == Structural highlights == | ||
| + | The <scene name='46/465442/Cv/10'>inhibitor of UK binds in the active site of UK</scene> and interacts with the active Ser of the catalytic triad<ref>PMID:19703768</ref>. Water molecules are shown as red spheres. | ||
== 3D Structures of urokinase == | == 3D Structures of urokinase == | ||
| + | [[Urokinase 3D Structures]] | ||
| + | </StructureSection> | ||
| + | ==References== | ||
| + | <references /> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
Current revision
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References
- ↑ Carriero MV, Stoppelli MP. The urokinase-type plasminogen activator and the generation of inhibitors of urokinase activity and signaling. Curr Pharm Des. 2011;17(19):1944-61. PMID:21711235
- ↑ Han B, Nakamura M, Mori I, Nakamura Y, Kakudo K. Urokinase-type plasminogen activator system and breast cancer (Review). Oncol Rep. 2005 Jul;14(1):105-12. PMID:15944776
- ↑ West CW, Adler M, Arnaiz D, Chen D, Chu K, Gualtieri G, Ho E, Huwe C, Light D, Phillips G, Pulk R, Sukovich D, Whitlow M, Yuan S, Bryant J. Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Bioorg Med Chem Lett. 2009 Oct 1;19(19):5712-5. Epub 2009 Aug 7. PMID:19703768 doi:10.1016/j.bmcl.2009.08.008
